Referenced in: none

Automatically associated channels: Kv11.1

Title: NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.

Authors: Georg Höfner, Cornelia E Hoesl, Chris Parsons, Günther Quack, Klaus T Wanner

Journal, date & volume: Bioorg. Med. Chem. Lett., 2005 May 2 , 15, 2231-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/15837299

Abstract
Enantiopure 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives were tested for their affinity to the ifenprodil binding site of the NMDA receptor, their potency to inhibit [3H]MK801 binding and their NMDA-NR2B subtype selectivity. The (1S,1'S)-configurated series displayed the highest affinity to the ifenprodil binding site. A reasonable potency and NMDA-NR2B subtype selectivity was found for (1S,1'S)-4c (R1=Me, R2=OMe). A high affinity to HERG K+ channels, however, suggests that (1S,1'S)-4c may involve an increased risk of cardiovascular side effects.